title: Phospholipid-functionalized mesoporous silica nanocarriers for selective photodynamic therapy of cancer.
abstract: This paper describes the fabrication of a highly efficient, non-cytotoxic drug delivery platform designed for photodynamic therapy (PDT): phospholipid-capped, protoporphyrin IX-loaded and FITC-sensitized mesoporous silica nanocarriers (Lipo-FMSNs/PpIX). After derivatization with folate on the phospholipid-capped FMSNs (denoted fa-Lipo-FMSNs/PpIX, the so-called nanoPDT system), we confirmed the nanoPDT systems' selective targeting of and entry into the folic acid receptor-overexpressed HeLa cells by means of cell viability assessment and confocal microscopic analysis. The decrease in the unfavorable dark toxicity of fa-Lipo-FMSNs/PpIX enabled the delivery of high concentrations of PpIX into cells. Moreover, the cellular uptake of the nanoPDT systems was greater than that of free PpIX. Upon irradiation with visible light, the nanoPDT system generated singlet oxygen efficaciously in aqueous environments-a decisive factor affecting its therapeutic applicability in PDT, demonstrating enhanced in vitro photocytotoxicity. Furthermore, an in vivo study of subcutaneous melanoma in nude mice inoculated with B16F10 cells revealed the capability for the nanoPDT system to mitigate nearly 65% of tumor growth.
authors.affiliation: Department of Chemistry, National Tsing Hua University, Hsinchu 30013, Taiwan.
authors.forename: I-Ting
authors.initials: IT
authors.lastname: Teng
authors.forename: Ya-Ju
authors.initials: YJ
authors.lastname: Chang
authors.forename: Li-Sheng
authors.initials: LS
authors.lastname: Wang
authors.forename: Hsin-Yi
authors.initials: HY
authors.lastname: Lu
authors.forename: Li-Chen
authors.initials: LC
authors.lastname: Wu
authors.forename: Chia-Min
authors.initials: CM
authors.lastname: Yang
authors.forename: Chih-Chung
authors.initials: CC
authors.lastname: Chiu
authors.forename: Chih-Hsueh
authors.initials: CH
authors.lastname: Yang
authors.forename: Shih-Lan
authors.initials: SL
authors.lastname: Hsu
authors.forename: Ja-an Annie
authors.initials: JA
authors.lastname: Ho
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers; D004705:Endocytosis; D005453:Fluorescence; D005492:Folic Acid / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D007150:Immunohistochemistry; D042541:Intracellular Space / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008546:Melanoma, Experimental / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D008819:Mice, Nude; D053758:Nanoparticles / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D010743:Phospholipids / Q000737:chemistry*; D010778:Photochemotherapy; D016062:Porosity; D011524:Protoporphyrins / Q000737:chemistry; D012822:Silicon Dioxide / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D010743:Phospholipids; D011524:Protoporphyrins; D012822:Silicon Dioxide; D005492:Folic Acid; C028025:protoporphyrin IX
keywords: Active targeting; Mesoporous silica nanoparticle; Phospholipid capping; Photocytotoxicity; Photodynamic cancer therapy